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PF 429242 dihydrochloride
Reversible, competitive inhibitor of sterol regulatory element-binding protein (SREBP) site 1 protease (IC50 = 0.175 μM). Selective for site 1 protease against a panel of serine proteases. Inhibits rate of cholesterol synthesis in CHO cells (IC50 = 0.53 μM). Also displays antiviral activity. Cell permeable.
Sold for research purposes under agreement from Pfizer Inc.
|Storage||Desiccate at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 482.49. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||4.15 mL||20.73 mL||41.45 mL|
|2.5 mM||0.83 mL||4.15 mL||8.29 mL|
|5 mM||0.41 mL||2.07 mL||4.15 mL|
|25 mM||0.08 mL||0.41 mL||0.83 mL|
References are publications that support the biological activity of the product.
Hay et al (2007) Aminopyrrolidineamide inhibitors of site-1 protease. Bioorg.Med.Chem.Lett. 17 4411 PMID: 17583500
Hawkins et al (2008) Pharmacologic inhibition of site 1 protease activity inhibits sterol regulatory element-binding protein processing and reduces lipogenic enzyme gene expression and lipid synthesis in cultured cells and experimental animals. J.Pharmacol.Exp.Ther. 326 801 PMID: 18577702
Urata et al (2011) Antiviral activity of a small-molecule inhibitor of arenavirus glycoprotein processing by the cellular site 1 protease. J.Virol. 85 795 PMID: 21068251
Olmstead (2012) Human subtilase SKI-1/S1P is a master regulator of the HCV lifecycle and a potential host cell target for developing indirect-acting antiviral agents. PLoS.Pathog. 8 e1002468 PMID: 22241994
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6 Citations for PF 429242 dihydrochloride
Citations are publications that use Tocris products. Selected citations for PF 429242 dihydrochloride include:
Flint et al (2019) A genome-wide CRISPR screen identifies N-acetylglucosamine-1-phosphate transferase as a potential antiviral target for Ebola virus. Nat Commun 10 285 PMID: 30655525
Tien et al (2019) Ambient particulate matter attenuates Sirtuin1 and augments SREBP1-PIR axis to induce human pulmonary fibroblast inflammation: molecular mechanism of microenvironment associated with COPD. Aging (Albany NY) 11 4654 PMID: 31299012
Urata et al (2015) Analysis of Assembly and Budding of Lujo Virus. J Virol 90 3257 PMID: 26719243
Scott et al (2018) TFAP2 transcription factors are regulators of lipid droplet biogenesis. Elife 7 PMID: 30256193
Uchida et al (2016) Suppressive effects of the site 1 protease (S1P) inhibitor, PF-429242, on dengue virus propagation. Viruses 8 E46 PMID: 26875984
Kleinfelter et al (2015) Haploid Genetic Screen Reveals a Profound and Direct Dependence on Cholesterol for Hantavirus Membrane Fusion. Ann Rheum Dis 6 e00801 PMID: 26126854
Do you know of a great paper that uses PF 429242 dihydrochloride from Tocris? Please let us know.
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Cancer Metabolism Poster
Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the main targets for cancer metabolism researchers. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways. These distinct metabolic circuits could provide viable cancer therapeutic targets.